Cell4Pharma ABC Transporter Vesicle Kits
HEK293-derived inside-out membrane vesicle kits for the full panel of regulatory ABC transporters — BSEP, BCRP, P-gp and MRP1–MRP5/MRP8 — for DDI studies and DILI risk assessment per FDA and EMA guidance.
Full Regulatory Panel
BSEP, BCRP, P-gp and MRP1–MRP5/MRP8 — the complete set of transporters referenced in FDA and EMA DDI guidance.
100 Reactions per Kit
Each kit is sized for 100 reactions in a 96-well plate format, suitable for IC50 determination and screening.
Inside-Out HEK293 Vesicles
Confirmed transporter expression and orientation for reliable, reproducible transport data.
Assay Service Available
Don't have in-house capacity? Our ciPTEC assay service can run the full transporter panel for you.
Kit specifications and guaranteed transport ratios
Every kit is released against a validated probe substrate with a specified minimum ATP/AMP transport ratio.
The ATP/AMP ratio is the practical quality metric for a vesicular transport assay. It expresses how much of the measured accumulation is genuine ATP-dependent transport rather than passive uptake and non-specific binding. A low ratio compresses the assay window and inflates IC50 variability — which is why it belongs on the datasheet rather than in the small print.
| Transporter | Probe substrate | ATP/AMP ratio |
|---|---|---|
| P-gp (MDR1, ABCB1) | Convallatoxin | > 5 |
| BSEP (ABCB11) | Taurocholate (TCA) | > 10 |
| BCRP (ABCG2) | Estrone-3-sulfate (E1S) | > 10 |
| MRP1 (ABCC1) | Estradiol-17β-glucuronide | > 5 |
| MRP2 (ABCC2) | CDCF | > 20 |
| MRP3 (ABCC3) | Estradiol-17β-glucuronide | > 10 |
| MRP4 (ABCC4) | DHEAS | > 5 |
| MRP5 (ABCC5) | CDCF | > 3 |
| MRP8 (ABCC11) | DHEAS | > 3 |
Lot-specific activity data is supplied with each kit. Control vesicles from non-transfected HEK293 cells are available separately and belong in every assay run — ATP-dependent transport is defined as the difference between the two.
Format and handling
- Ready on thawing. No expansion, no differentiation, no monolayer to qualify — the vesicles go straight from −80 °C into the assay.
- Robust to handling. Transport activity is retained after storage at −20 °C, after two days at 4 °C, and across five freeze-thaw cycles.
- Detection-agnostic. Compatible with radiolabel, LC-MS/MS and fluorescence readouts — see the detection method comparison.
- EU stock. Supplied from Europe for the DACH region — no US import lead time or customs delay.
Why ABC transporter testing matters in DMPK programs
ABC (ATP-binding cassette) transporters mediate the efflux of drugs and metabolites across cell membranes, and inhibition of key transporters — particularly BSEP, BCRP and P-gp — is mechanistically linked to drug-induced liver injury (DILI) and clinically relevant drug-drug interactions (DDI). FDA and EMA guidance both recommend transporter inhibition testing as part of standard DMPK characterisation.
The vesicle-based assay format uses HEK293-derived inside-out membrane vesicles with confirmed transporter expression, allowing direct measurement of transporter-mediated substrate uptake in the presence and absence of test compounds — the basis for IC50 determination and single-concentration screening.
Because inhibition of multiple transporters can compound DILI risk — for example, BSEP inhibition together with MRP2, MRP3 or MRP4 impairs the compensatory bile acid efflux pathways that partially protect hepatocytes — a full panel typically gives a more complete risk picture than testing BSEP in isolation.
Typical applications
- Drug-induced liver injury (DILI) risk assessment
- Drug-drug interaction (DDI) studies per FDA/EMA guidance
- Hepatotoxicity screening in lead optimisation
- IC50 determination for transporter inhibitors
- Regulatory submission transporter panels
- Academic and pharmaceutical DMPK research
ABC Transporter Vesicle Kits — Overview
Choose the transporter kit matched to your study. Bulk pricing and full panel quotes are available on request.
BSEP Vesicle Kit
Bile salt export pump — DILI and cholestasis risk assessment.
Learn more →BCRP Vesicle Kit
Breast cancer resistance protein — FDA/EMA core panel transporter.
Learn more →P-gp Vesicle Kit
P-glycoprotein — the most widely tested efflux transporter.
Learn more →MRP1 Vesicle Kit
Multidrug resistance protein 1 — broad substrate efflux transporter.
Learn more →MRP2 Vesicle Kit
Hepatic canalicular transporter — relevant to BSEP-related DILI risk.
Learn more →MRP3 Vesicle Kit
Basolateral hepatic transporter — compensatory bile acid efflux.
Learn more →MRP4 Vesicle Kit
Nucleotide and bile acid efflux transporter, broad tissue expression.
Learn more →MRP5 Vesicle Kit
Cyclic nucleotide efflux transporter, relevant to nucleotide analogues.
Learn more →MRP8 Vesicle Kit
ABCC11 transporter — relevant to specific drug efflux studies.
Learn more →Control Vesicle Kit
Non-transfected control vesicles for background and specificity controls.
Learn more →Need a quote for a full transporter panel?
Contact our team for pricing, technical documentation and assay support across the full ABC transporter vesicle kit range.
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